WO 2002/060872 (PCT/AU2002/000099) and WO 2007/087684 (PCT/AU2007/000101) discloses, inter alia, substituted benzofuran compounds of the following general class:

These compounds have been shown to possess promising anti-proliferative activity as tubulin polymerisation inhibitors (TPIs)
While the synthesis of the 2-aryl-3-aroyl-benzofuran class has been quite successful on a laboratory scale (that is, less than 10 gram scale) the use of this methodology to efficiently produce larger amounts (i.e., kilogram scale) of this and other preferred 2-substituted 3-aroyl-benzofurans has proven to be challenging. This has caused the present inventors to devise new scale up methodology to overcome the current deficiencies which exist in the art. The present invention is directed to addressing these shortcomings to enable an efficient kilogram scale synthesis of a preferred class of substituted benzofurans which display unique TPI activity.